The present disclosure provides a preparation method for m-diamide compounds. The method includes the following steps: 2-fluoro-3-nitrobenzoyl chloride and 4-(perfluoropropane-2-yl)-2-(trifluoromethyl)aniline are subjected to a condensation reaction, followed by a reduction reaction and an alkylation reaction to give 2-fluoro-3-(alkylamino)-N-(4-(perfluoropropane-2-yl)-2-(trifluoromethyl)phenyl)benzamide, which reacts with an acyl chloride compound to give 2-fluoro-3-(alkylbenzamido)-N-(4-(perfluoropropane-2-yl)-2-(trifluoromethyl)phenyl)benzamide, which is finally brominated to obtain the m-diamide compound. The reactions are almost quantitative with few by-products. Cryogenic and high-temperature reactions are not used. The introduction of bromine atoms at specific sites can be achieved in the final step. The preparation method has high yield and is more suitable for industrial production.

The present disclosure provides a preparation method for m-diamide compounds. The method includes the following steps: 2-fluoro-3-nitrobenzoyl chloride and 4-(perfluoropropane-2-yl)-2-(trifluoromethyl)aniline are subjected to a condensation reaction, followed by a reduction reaction and an alkylation reaction to give 2-fluoro-3-(alkylamino)-N-(4-(perfluoropropane-2-yl)-2-(trifluoromethyl)phenyl)benzamide, which reacts with an acyl chloride compound to give 2-fluoro-3-(alkylbenzamido)-N-(4-(perfluoropropane-2-yl)-2-(trifluoromethyl)phenyl)benzamide, which is finally brominated to obtain the m-diamide compound. The reactions are almost quantitative with few by-products. Cryogenic and high-temperature reactions are not used. The introduction of bromine atoms at specific sites can be achieved in the final step. The preparation method has high yield and is more suitable for industrial production.

The present invention relates to hyper-branched compounds, a method of synthesizing the hyper-branched compounds and applications of the hyper-branched compounds. The hyper-branched compounds of the present invention include hyper-branched fluorinated compounds, hyper-branched fluorinated graphene and hyper-branched amine functionalized graphene oxide.

The present invention relates to new compounds of formula (I) that show great affinity and activity towards the subunit 2 of voltage-gated calcium channels (VGCC), especially the 2-1 subunit of voltage-gated calcium channels or dual activity towards the subunit 2 of voltage-gated calcium channels (VGCC), especially the 2-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.

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Provided is a method for preparing an N-cyclopropylmethyl aniline compound, which comprises reacting a compound represented by Formula IV with cyclopropyl formaldehyde in the presence of metal zinc and an acid to generate an N-cyclopropylmethyl aniline compound represented by Formula I. The method of the present disclosure has mild reaction conditions, short reaction time, a high yield, simple processes, simple operations and low costs, and is more applicable to industrial production.

Provided is a method for preparing an N-cyclopropylmethyl aniline compound, which comprises reacting a compound represented by Formula IV with cyclopropyl formaldehyde in the presence of metal zinc and an acid to generate an N-cyclopropylmethyl aniline compound represented by Formula I. The method of the present disclosure has mild reaction conditions, short reaction time, a high yield, simple processes, simple operations and low costs, and is more applicable to industrial production.

In accordance with one or more embodiments, the present invention provides a compound of formulas I, II, and III, for use in methods of inhibition of PBX1-DNA interaction in a mammalian cell or population of cells, and for use in the treatment of medical conditions including but not limited to cancers, developmental disorders, inflammatory disorders, autoimmune diseases, or neuro-degenerative disorders.

In accordance with one or more embodiments, the present invention provides a compound of formulas I, II, and III, for use in methods of inhibition of PBX1-DNA interaction in a mammalian cell or population of cells, and for use in the treatment of medical conditions including but not limited to cancers, developmental disorders, inflammatory disorders, autoimmune diseases, or neuro-degenerative disorders.

The present invention relates generally to glutaminase inhibitors of Formula I, Formula II, or Formula III, as well as pharmaceutical compounds containing them and methods of their use.

The present invention relates generally to glutaminase inhibitors of Formula I, Formula II, or Formula III, as well as pharmaceutical compounds containing them and methods of their use.